Gang L Liu

US Patent:

6353109, Mar 5, 2002

Filed:

Jun 1, 1998

Appl. No.:

09/088522

Inventors:

Pamela Albaugh - Clinton CT
Gang Liu - Branford CT
Alan Hutchison - Madison CT

Assignee:

Neurogen Corporation - Branford CT

International Classification:

C07C23359

US Classification:

5462774, 5462777, 5462781, 548492, 548504, 548512, 548516, 564163, 564169, 564172, 564180, 564189

Abstract:

Disclosed are compounds of the formula or the pharmaceutically acceptable non-toxic salts thereof wherein: W represents substituted or unsubstituted aryl or heteroaryl; T is hydrogen, halogen, hydroxyl, amino or alkyl; X is hydrogen, hydroxy, or lower alkyl; m is 0, 1, or 2; n is 0, 1, or 2; and R and R represent substituted or unsubstituted organic residues. These compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors. These compounds are useful in the diagnosis and treatment of anxiety, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory.

US Patent:

6380209, Apr 30, 2002

Filed:

May 30, 2000

Appl. No.:

09/583147

Inventors:

Guolin Cai - Guilford CT
Gang Liu - Agoura CA

Assignee:

Neurogen Corporation - Branford CT

International Classification:

A61K 314375

US Classification:

514300, 514301, 514258, 514249, 514248, 544236, 544279, 544350, 546114, 546122

Abstract:

Disclosed are compounds of the formula or the pharmaceutically acceptable non-toxic salts thereof wherein: R is hydrogen, alkyl, or(un)substituted alkoxy or amino; and W is (un)substituted alkyl, aryl, or heteroaryl, which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors. The compounds of the invention are useful in the diagnosis and treatment of anxiety, Down Syndrome, sleep, cognitive and seizure disorders, and overdose with benzodiazepine drugs and for enhancement of alertness.

US Patent:

6399604, Jun 4, 2002

Filed:

Aug 8, 2000

Appl. No.:

09/634093

Inventors:

Pamela A. Albaugh - Clinton CT
Robert W. DeSimone - Durham CT
Gang Liu - Agoura CA

Assignee:

Neurogen Corporation - Branford CT

International Classification:

A61K 31535

US Classification:

5142352, 514300, 544128, 546123

Abstract:

The present invention encompasses structures of the Formula or the pharmaceutically acceptable non-toxic salts thereof wherein: X is hydrogen, halogen, (un)substituted alkyl, (un)substituted alkoxy or amino; and Y is (un)substituted alkyl, aryl, or heteroaryl, which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors. These compounds are useful in the diagnosis and treatment of anxiety, Down Syndrome, sleep, cognitive and seizure disorders, and overdose with benzodiazepine drugs and for enhancement of alertness.

US Patent:

6423711, Jul 23, 2002

Filed:

Dec 13, 2000

Appl. No.:

09/736497

Inventors:

Guolin Cai - Guilford CT
Gang Liu - Agoura CA
Guoquing Chen - North Branford CT
Pamela A. Albaugh - Clinton CT

Assignee:

Neurogen Corporation - Branford CT

International Classification:

C07D41304

US Classification:

5142338, 51425304, 514301, 544127, 544362, 546114

Abstract:

Disclosed are compounds of the formula or the pharmaceutically acceptable non-toxic salts thereof wherein: n is an integer from 0 to 3; the C ring is aryl or heteroaryl; X is CH, N, or O Z represents an electron pair, hydrogen, or (un)substituted heterocycle, aryl, or amido; W is (un)substituted alkyl, aryl, or heteroaryl; A and B are hydrogen or lower alkyl, which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors. These compounds are useful in the diagnosis and treatment of anxiety, Down Syndrome, sleep, cognitive and seizure disorders, and overdose with benzodiazepine drugs and for enhancement of alertness.

US Patent:

6448246, Sep 10, 2002

Filed:

May 25, 2000

Appl. No.:

09/578928

Inventors:

Guolin Cai - Guilford CT
Gang Liu - Agoura CA
Pamela A. Albaugh - Clinton CT

Assignee:

Neurogen Corporation - Branford CT

International Classification:

C07D27916

US Classification:

5142242, 544 51, 544 52

Abstract:

Disclosed are 4H-1,4-Benzothiazine-2-carboxamides. These compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors. These compounds are useful in the diagnosis and treatment of anxiety, depression, sleep, cognitive and seizure disorders, and overdose with benzodiazepine drugs and for enhancement of alertness. Pharmaceutical compositions, including packaged pharmaceutical compositions, are further provided. Compounds of the invention are also useful as probes for the localization of GABAA receptors in tissue samples.

US Patent:

6515140, Feb 4, 2003

Filed:

Mar 8, 2001

Appl. No.:

09/801956

Inventors:

Pamela Albaugh - Clinton CT
Gang Liu - Agoura CA
Kenneth Shaw - Weston CT
Alan Hutchison - Madison CT

Assignee:

Neurogen Corporation - Branford CT

International Classification:

C07D40312

US Classification:

548455, 548454, 544105

Abstract:

Disclosed are compounds of the formula: or the pharmaceutically acceptable non-toxic salts thereof wherein: G, X, T, n, and R -R are as defined herein, which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors. These compounds are useful in the diagnosis and treatment of anxiety, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory.

US Patent:

61437603, Nov 7, 2000

Filed:

Aug 25, 1998

Appl. No.:

9/139456

Inventors:

Pamela A. Albaugh - Clinton CT
Robert W. DeSimone - Durham CT
Gang Liu - Agoura CA

Assignee:

Neurogen Corporation - Branford CT

International Classification:

A61K 3144
C07D47102

US Classification:

514300

Abstract:

The present invention encompasses structures of the Formula ##STR1## or the pharmaceutically acceptable non-toxic salts thereof wherein: x is hydrogen, halogen, (un)substituted alkyl, (un)substituted alkoxy or amino; and Y is (un)substituted alkyl, aryl, or heteroaryl, which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors. These compounds are useful in the diagnosis and treatment of anxiety, Down Syndrome, sleep, cognitive and seizure disorders, and overdose with benzodiazepine drugs and for enhancement of alertness.

US Patent:

6080873, Jun 27, 2000

Filed:

Sep 4, 1998

Appl. No.:

9/148247

Inventors:

Pamela Albaugh - Clinton CT
Gang Liu - Branford CT
Kenneth Shaw - Weston CT
Alan Hutchison - Madison CT

Assignee:

Neurogen Corporation - Branford CT

International Classification:

C07D20914
C07D20934
C07D20940

US Classification:

548516

Abstract:

The present invention encompasses structures of the formula I: ##STR1## or the pharmaceutically acceptable non-toxic salts thereof wherein: G represents ##STR2## where Q is aryl substituents optionally mono or disubstituted with hydroxy or halogen; T is halogen, hydrogen, hydroxyl, amino or alkoxy having 1-6 carbon atoms; W is oxygen, nitrogen, sulfur, or optionally substituted methylene; X is hydrogen, hydroxyl, or alkyl; Z is an organic or inorganic substituent optionally forming a ring with subtituents on Q; ##STR3## independently represent optionally substituted carbon chains; wherein k, m, and n are independently 0, or an integer of from 1-3 R. sub. 3, R. sub. 4, R. sub. 5, and R. sub. 6 are the same or different and represent organic or inorganic substituents. These compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors.